Ralaniten acetate
Ralaniten acetate (also known as EPI-506) is an androgen receptor antagonist which is under development by ESSA Pharma for the treatment of prostate cancer. It is a prodrug of ralaniten (EPI-002).
Mechanism of action[edit | edit source]
Ralaniten acetate acts by binding to the N-terminal domain of the androgen receptor (AR). This is in contrast to other AR antagonists like bicalutamide and enzalutamide, which bind to the C-terminal ligand-binding domain of the AR. The N-terminal domain is where the AR is activated by coactivator proteins. By binding to this site, ralaniten acetate prevents the AR from being activated by these coactivators.
Clinical trials[edit | edit source]
Ralaniten acetate has been studied in a phase I/II clinical trial for prostate cancer. The results of this trial have not yet been published.
See also[edit | edit source]
References[edit | edit source]
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